化合物信息

Drug Groups

approved

Description

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve the symptoms of arthritis, primary dysmenorrhea, fever; and as an analgesic, especially where there is an inflammatory component. It is closely related to piroxicam. In Europe it is marketed under the brand names Movalis, Melox, and Recoxa. In North America it is generally marketed under the brand name Mobic. In Latin America, the drug is marketed as Tenaron. [Wikipedia]

Indication

For symptomatic treatment of arthritis and osteoarthritis.

Pharmacology

Meloxicam is an nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Prostaglandins are substances that contribute to inflammation of joints. Meloxicam inhibits prostaglandin synthetase (cylooxygenase 1 and 2) and leads to a decrease of the synthesis of prostaglandins, therefore, inflammation is reduced.

Toxicity

LD₅₀, Acute: 84 mg/kg (Rat); Oral 470 mg/kg (Mouse); Oral 320 mg/kg (Rabbit)

Affected Organisms

Biotransformation

Meloxicam is almost completely metabolized into inactive metabolites by the cytochrome P450 (CYP450) isozymes. CYP2C9 is primarily responsible for metabolism of meloxicam while CYP3A4 plays a minor role. An intermediate metabolite, 5'-hydroxymethyl meloxicam, is further metabolized to 5'-carboxy meloxicam, the major metabolite. Peroxidase activity is thought to produce the two other inactive metabolites of meloxicam.

Absorption

Absolute bioavailability = 89%

Half Life

15-20 hours

Protein Binding

99.4% bound, primarily to albumin

Elimination

Meloxicam is almost completely metabolized to four pharmacologically inactive metabolites. Meloxicam excretion is predominantly in the form of metabolites, and occurs to equal extents in the urine and feces. Only traces of the unchanged parent compound are excreted in the urine (0.2%) and feces (1.6%). The extent of the urinary excretion was confirmed for unlabeled multiple 7.5 mg doses: 0.5%, 6% and 13% of the dose were found in urine in the form of meloxicam, and the 5'-hydroxymethyl and 5'-carboxy metabolites, respectively.

Distribution

* 10 L

Clearance

* 8.8 mL/min [Healthy Male Adults (Fed) oral 7.5 mg tablets]
* 9.9 mL/min [Eldery Male (Fed) oral 15 mg capsules]
* 5.1 mL/min [Eldery Female (Fed) oral 15 mg capsules]
* 19 mL/min [Renal Failure (Fasted) oral 15 mg capsules]
* 11 mL/min [Hepatic Insufficiency (Fasted) oral 15 mg capsules]

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